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Pharmacokinetics, clinical indications, and resistance mechanisms in molecular targeted therapies in cancer

Benjamin Izar1, Julia Rotow, Justin Gainor

  • 110 North Grove Street, LRH 214, Boston, MA, 02114. bchabner@partners.org.

Pharmacological Reviews
|October 5, 2013
PubMed

Insights

New cancer drug development focuses on targeted therapies, not just cytotoxic agents. This review covers FDA-approved targeted cancer drugs, their clinical trials, and mechanisms of resistance.

Area of Science:

  • Oncology
  • Pharmacology
  • Drug Development

Background:

  • Cancer treatment has evolved from cytotoxic agents to targeted therapies.
  • Targeted therapies selectively inhibit oncogenic drivers in various cancers.
  • Significant advancements in targeted cancer therapies have emerged in the last decade.

Purpose of the Study:

  • To review the clinical pharmacokinetic characteristics of FDA-approved targeted cancer therapies.
  • To provide an overview of pivotal clinical trials leading to drug approvals.
  • To describe resistance mechanisms against targeted cancer treatments.

Main Methods:

  • Literature review of U.S. Food and Drug Administration (FDA) approved targeted therapies.
  • Analysis of clinical pharmacokinetic data.
  • Summary of key clinical trial outcomes.
  • Description of general and specific resistance principles and mechanisms.

Main Results:

  • Numerous targeted therapies are now approved for hematological and solid malignancies.
  • Pharmacokinetic profiles and clinical trial data support their efficacy.
  • Development of resistance is a major challenge in targeted cancer therapy.
  • Specific resistance mechanisms have been identified for several targeted agents.

Conclusions:

  • Targeted cancer therapies represent a paradigm shift in oncology.
  • Understanding pharmacokinetics and resistance is crucial for optimizing treatment.
  • Continued research into overcoming resistance is essential for improving patient outcomes.

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